Unicontin

Unicontin is a remedy that affects the respiratory system, based on theophylline. It is often used in medical practice in cases of obstruction of the respiratory tract. Medicinal accessory: antispasmodics, xanthines. 

Unicontin is not available in the public domain and is only available on prescription from a doctor. 

Indications Unicontin

Unicontin is prescribed for obstructive pulmonary pathologies:

• with bronchial asthma;
• with chronic obstructive bronchitis;
• with pulmonary emphysema.

Also, the drug can be used for the complex treatment of pulmonary hypertension, "pulmonary heart", nocturnal apnea. 

[1]

Release form

Unicontin is available in tablet form in a dosage of 400 or 600 mg.

Tablet 400 mg light, rounded, flattened, has a separation notch on one side, as well as engraving MM and U / 400.

Tablet 600 mg white, oblong, convex on both sides, has a separation incision and engraving MM and U / 600.

The blister contains 10 tablets. The package consists of 10 blisters.

Unicontin refers to long-acting drugs. Each tablet consists of an active component of theophylline, as well as additional ingredients: povidone, hydroxyethylcellulose, cetostearyl alcohol, talc, magnesium stearate.

[2]

Pharmacodynamics

Active substance Unikontin refers to bronchodilators from a number of methylxanthines. It has a stimulating effect on the central nervous system, cardiac muscle and skeletal muscles, facilitates the removal of spasms of smooth muscle fibers, and is also an easy diuretic.

The mechanism of action of the active component is based on its property to suppress the enzyme phosphodiesterase. Theophylline also influences the smooth muscle structures of the coronary arteries, the blood supply of the muscular system and lobes, has a relaxing effect on the uterine musculature, sphincters of the esophagus and bile ducts.

Unicontin improves the excretion of blood from the right ventricle, which has a positive effect on the degree of cardiac output, on lowering resistance in the vascular system of the lungs and reducing intrapulmonary pressure. Simultaneously, the respiratory center is stimulated, the muscles of the diaphragm are activated, the excretion of urine increases, and the production of catecholamines by the adrenals is increased.

The peak efficiency is observed when a concentrated amount of plasma is reached from 5 to 20 μg / ml. 

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Pharmacokinetics

Pharmacokinetic properties of Unicontin may differ depending on the individual characteristics of the patient, since the presence of additional pathologies and the intake of certain drugs can significantly affect kinetic mechanisms. For this reason, experts recommend keeping the amount of medication in the blood serum under control, especially in patients with severe diseases or with prolonged treatment with this drug.

Active ingredient Unicontin is well absorbed in the digestive system. The constant content of the active ingredient is established already 2-3 days after the start of the drug intake. Theophylline soon spreads practically to all tissues and biological environments of the body. Metabolism is carried out in the liver, while one of the metabolic products also has a bronchodilating ability.

The exchange products and the remains of the active ingredient are excreted through the urinary system.

[4], [5]

Dosing and administration

Dosing Unicontin is prescribed strictly individually, which is associated with some features of the patient's metabolism, their age and weight category. A tablet is taken once a day (in the morning or in the evening), during a meal. If the patient has taken the first dose of medication on an empty stomach, then in the future he should adhere to this particular regimen.

The tablet is taken whole, without crushing and chewing. If necessary, the tablet can be divided according to a specially applied incision.

The initial dosage of the drug for patients with normal creatinine clearance:

Periodicity of change of dosage	Children weighing less than 45 kg	Children weighing more than 45 kg and adults
Initial dosage	From 12 to 14 mg / kg / day, but not more than 300 mg / day	300 to 400 mg / day
After 3 days, the dosage is increased	16 mg / kg / day, but not more than 400 mg / day	From 400 to 600 mg / day
After 3 days, if necessary	20 mg / kg / day, but not more than 600 mg / day	If necessary, appoint more than 600 mg / day under strict control of serum concentration

In case of violations of creatinine clearance, the dosage of medication in pediatrics in patients under 15 years of age should not exceed 16 mg / kg / day (but not more than 400 mg / day).

In patients with changes in creatinine clearance from 16 years of age and older, the dosage of the drug per day should not be more than 400 mg.

Selection of dosage depending on the content of medication in the blood serum:

Limit serum concentrations of medication	Dosage selection
Less than 9.9 μg ml	If the drug is not effective, you can increase the dosage by 25%.
10 to 14.9 μg / ml	The current dosage is prescribed with repeated analyzes of the concentrations every six months or a year.
15 to 19.9 μg ml	One should consider reducing the dosage of Unicontin by 10%, even if its tolerability is normal.
From 20 to 24.9 μg ml	It is necessary to reduce the dosage of Unicontin by 25% even with normal tolerability, with repeated concentration analysis after 3 days.
From 25 to 30 μg / ml	It is necessary to skip one dose of the drug, and lower the following dosages by 25%. After 3 days, re-assay the concentration.
More than 30 μg / ml	Dosage should be reduced minimally by 50%, followed by a re-analysis of the content after 3 days.

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Use Unicontin during pregnancy

It is proved that this Unicontin is able to pass through the placental barrier and be determined in the mother's milk.

During pregnancy, Unicontin can be administered only if the intended benefit for a woman is more important than the possible risk to a future baby. If the drug was still prescribed to a pregnant woman, the treatment is carried out under the constant control of the level of active substance in the blood plasma, which will allow to carefully adjust the dosage. It is recommended to refrain from treatment with this medication late in pregnancy, because of its ability to prevent generic uterine contractions.

At thoracal feeding the woman should closely watch a status of the kid for occurrence at it or him allergic reaction to a preparation, excessive exaltation or a sleeplessness. If such symptoms appear, you should immediately consult a doctor who will make a decision, either to cancel Unicontin, or to stop lactation.

Contraindications

• Allergic sensitivity to any of the components of the medication, or to the preparations of the xanthine group.
• Acute period of myocardial infarction.
• Tachycardia with heart failure.
• Hypertrophy of the myocardium, obstructive form of cardiomyopathy.
• Hypertonic disease.
• Propensity to epilepsy.
• Increased functionality of the thyroid gland.
• Gastric ulcer and 12 duodenal ulcer.
• Severe hepatic insufficiency.
• Children under 12 years.

Side effects Unicontin

At the initial stages of treatment, occasional minor side effects can sometimes be observed:

• the appearance of heartburn, nausea, diarrhea, pain in the abdomen;
• cardiopalmus;
• dizziness, headaches, sleep disorders, feelings of anxiety, excitement, irritability;
• allergic manifestations in the form of skin rashes, itching and redness of the skin.

In more severe cases, as well as in especially sensitive patients, a sharp drop in blood pressure, a disorder of the heart rhythm, the appearance of trembling in the hands, convulsions, sleep disturbances are possible. Sometimes the body temperature may rise, diuresis may increase.

In the blood, hypokalemia, hypercalcemia, hyperglycemia, and also a high content of urate salts are found. 

Overdose

Symptoms of taking an excessive dose may be manifested when the active substance content in the blood serum is more than 110 μmol / liter.

A typical picture can be as follows:

• trembling in the limbs;
• attacks of nausea and vomiting;
• tenderness in the epigastric region;
• diarrhea;
• rave;
• heart rhythm disorders;
• hypotension;
• convulsions.

Symptoms of overdose may appear unexpectedly, without prior deterioration.

As a help, it is often sufficient to reduce the dosage or suspend the medication temporarily. If the violations are positioned as severe, then the dosage is reduced gradually, under the control of the concentration of the active component in the blood plasma.

In cases of intoxication, gastric lavage is prescribed with further intake of sorbent preparations.

During the entire recovery period, it is necessary to monitor blood pressure, heart rate and respiratory movements, as well as the active component content in the plasma.

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Interactions with other drugs

During the course of Unicontin therapy, the use of alcoholic beverages is prohibited. Also, products and liquids containing methylxanthine, which is present in coffee beverages, strong tea, cocoa, chocolate, chocolate products, should be restricted.

The effect of Unicontin may be more pronounced when taken concurrently with allopurinol, cimetidine, phenylbutazone, fluoroquinolone, furosemide, isoniazid, calcium antagonists, lincomycin, macrolide antibiotics, paracetamol, pentoxifylline, oral contraceptives, propranolol, ranitidine, and anti-influenza serum. When combined with any of these drugs, it is important to periodically analyze the content of the active ingredient Unicontin in serum.

When taking Ciprofloxacin at one stage, the dosage of Unicontin should be reduced by approximately 60%, and when Enoxacin is taken, it should be reduced by 30%.

The effect of Unicontin decreases with the simultaneous use of antiepileptic drugs, hypnotics, magnesium hydroxide, rifampicin, nicotine.

Unicontin may become ineffective when taken together with β-receptor antagonists.

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Storage conditions

The drug is stored at a temperature of no more than + 25 ° C, in a place protected from sunlight, out of the reach of children. 

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Shelf life

Shelf life of the medication is up to 3 years.

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